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August 28, 2011 Structure – Activity Relationships of Pyrrole Based S-Nitrosoglutathione Reductase Inhibitors – Carboxamide Modification
Xicheng Sun, Jian Qiu, Sarah A. Strong, Louis S. Green, Jan W. F. Wasley, Dorothy B. Colagiovanni,
Sarah C. Mutka, Joan P. Blonder, Adam M. Stout, Jane P. Richards, Lawrence Chun, and Gary J. Rosenthal
The enzyme S-nitrosoglutathione reductase (GSNOR) is a member of the alcohol dehydrogenase family (ADH) that regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO).
GSNO and SNOs are implicated in the pathogenesis of many diseases including those in respiratory, cardiovascular, and gastrointestinal systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently in clinical development for acute asthma.
We describe here the synthesis and structure activity relationships (SAR) of novel pyrrole based analogues of N6022 focusing on carboxamide modifications.
We have identified potent and novel GSNOR inhibitors that demonstrate efficacy in an ovalbumin (OVA) induced asthma model in mice. More…poster PDF(182Kb)
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